Lipid nano-pellets as excipient system for perorally administered drugs

Abstract

An excipient system containing a drug for peroral administration in the form of an ultrafine aqueous, colloidal suspension of lipid nano-pellets comprised of lipids and a surfactant of which the particle diameters of the nano-pellets range from 50-1,000 nm, preferably from 80-800 nm, the ratio of lipid to surfactant in the lipid nano-pellets ranging from 1:0.1 to 1:2.2, preferably from 1:0.22 to 1:1.2, especially from 1:1 to 1:0.22, and where the lipid nano-pellets are present in the suspension in a concentration of from 1-20% by weight. The lipid nano-pellets can be provided with pharmacologically active substances, making possible improved biological availability upon peroral administration.

What is claimed is: 
     
       1. An excipient system containing a pharmacologically effective substance for peroral administration characterized in that the excipient system comprises lipid nano-pellets having a particle size of from about 50 to 1000 nm in the form of an aqueous, colloidal suspension, the lipid particles being present in the suspension in a concentration of from about 1 to 20% by weight, said lipid particles consisting of a mixture of at least one lipid and at least one surfactant in a ratio of from about 1:0.1 to 1:2.2, respectively, said particles consisting of from about 5 to 70%.by weight of at least one lipid, from about 0.01 to 70% by weight of at least one surfactant, and from about 0.05 to 25% by weight of a pharmacologically effective substance. 
     
     
       2. The excipient system of claim 1 wherein said lipid nano-pellets have a particles size of from about 80 to 800 nm. 
     
     
       3. The excipient system of claim 1 wherein said at least one lipid and at least one surfactant are present in a ratio of from about 1:0.22 to 1:1.2. 
     
     
       4. The excipient system of claim 1 wherein said lipid at least one lipid and at least one surfactant are present in a ratio of from about 1:1 to 1:0.22. 
     
     
       5. The excipient system of claim 1 wherein said at east one lipid is selected from the group consisting of fatty alcohols of from 12 to 30 carbon atoms and their mono, di and triesters of glycerin and polyvalent alcohols. 
     
     
       6. The excipient system of claim 5 wherein said polyvalent alcohol is selected from the group consisting of ethylene glycol, propylene glycol, mannitol and sorbitol. 
     
     
       7. The excipient system of claim 1 wherein said at least one lipid is a fatty alcohol selected from the group consisting of lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, arachidyl alcohol and behenyl alcohol. 
     
     
       8. The excipient system of claim 1 wherein said at least one lipid is selected from the group consisting of lignoceryl alcohol, ceryl alcohol, cerotyl alcohol and myricyl alcohol. 
     
     
       9. The excipient system of claim 1 wherein said at least one lipid is a mixture of lipids. 
     
     
       10. The excipient system of claim 1 wherein said at least one surfactant comprises a natural bile salt. 
     
     
       11. The excipient system of claim 1 wherein said at least one surfactant is selected from the group consisting of sodium cholate, sodium dehydrocholate, sodium deoxycholate, sodium glycocholate, sodium laurocholate and mixtures thereof. 
     
     
       12. The excipient system of claim 1 wherein said at least one surfactant is selected from the group consisting of salts of sulfo-succinic acid esters, polyoxyethylene sorbitane esters, sorbitane esters, sorbitane ethers, polyoxyethylene fatty alcohol ethers, polyoxyethylene stearic acid esters, mixed condensates of polyoxyethylene ethers with polyoxypropylene ethers, ethoxylated saturated glycerides, partial fatty acid glycerides and polyglycides. 
     
     
       13. The excipient system of claim 1 wherein said at least one surfactant is a mixture of surfactants. 
     
     
       14. The excipient system of claim 1 wherein said lipid particles are present in said suspension in an amount of from about 8 to 15% by weight. 
     
     
       15. The excipient system of claim 14 wherein said lipid particles are present in said suspension in an amount of about 10% by weight. 
     
     
       16. An excipient system containing a pharmacologically effective substance for peroral administration characterized in that the excipient system comprises lipid nano-pellets having a particle size of from about 50 to 1000 nm, said lipid particles consisting of a mixture of at least one lipid and at least one surfactant in a ratio of from about 1:0.1 to 1:2.2, respectively, said particles consisting of from about 5 to 70% by weight of at least one lipid, from about 0.01 to 70% by weight of at least one surfactant, and from about 0.05 to 25% by weight of a pharmacologically effective substance. 
     
     
       17. The excipient system of claim 16 wherein said lipid nano-pellets have a particles size of from about 80 to 800 nm. 
     
     
       18. The excipient system of claim 16 wherein said at least one lipid and at least one surfactant are present in a ratio of from about 1:0.22 to 1:1.2. 
     
     
       19. The excipient system of claim 16 wherein said lipid at least one lipid and at least one surfactant are present in a ratio of from about 1:1 to 1:0.22. 
     
     
       20. The excipient system of claim 16 wherein said at least one lipid is selected from the group consisting of fatty alcohols of from 12 to 30 carbon atoms and their mono, di and triesters of glycerin and polyvalent alcohols. 
     
     
       21. The excipient system of claim 20 wherein said polyvalent alcohol is selected from the group consisting of ethylene glycol, propylene glycol, mannitol and sorbitol. 
     
     
       22. The excipient system of claim 16 wherein said at least one lipid is a fatty alcohol selected from the group consisting of lauryl alcohol, myristyl alcohol, cetyl alcohol, stearyl alcohol, arachidyl alcohol and behenyl alcohol. 
     
     
       23. The excipient system of claim 16 wherein said at least one lipid is selected from the group consisting of lignoceryl alcohol, ceryl alcohol, cerotyl alcohol and myricyl alcohol. 
     
     
       24. The excipient system of claim 16 wherein said at least one lipid is a mixture of lipids. 
     
     
       25. The excipient system of claim 16 wherein said at least one surfactant comprises a natural bile salt. 
     
     
       26. The excipient system of claim 16 wherein said at least one surfactant is selected from the group consisting of sodium cholate, sodium dehydrocholate, sodium deoxycholate, sodium glycocholate, sodium laurocholate and mixtures thereof. 
     
     
       27. The excipient system of claim 16 wherein said at least one surfactant is selected from the group consisting of salts of sulfo-succinic acid esters, polyoxythylene sorbitane esters, sorbitane esters, sorbitane ethers, polyoxyethylene fatty alcohol ethers, polyoxyethylene stearic acid esters, mixed condensates of polyoxyethylene ethers with polyoxypropylene ethers, ethoxylated saturated glycerides, partial fatty acid glycerides and polyglycides. 
     
     
       28. The excipient system of claim 16 wherein said at least one surfactant is a mixture of surfactants.